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R-30490 (also known as 4-Methoxymethylfentanyl) is an opioid analgesic related to the highly potent animal tranquilizer carfentanil, and with only slightly lower potency.
It was first synthesised by a team of chemists at Janssen Pharmaceutica led by Paul Janssen, who were investigating the structure-activity relationships of the fentanyl family of drugs.
R-30490 was found to be the most selective agonist for the μ-opioid receptor out of all the fentanyl analogues tested, but it has never been introduced for medical use in humans, although the closely related drug sufentanil is widely used for analgesia and anesthesia during major surgery.
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Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear
Carfentanil was sold starting in 1986 under the brand name “Wildnil” for use in tranquilizer darts in combination with an α2-adrenoreceptor agonist:9 for large mammals including elk and elephants.
Radiolabelled [11C]carfentanil is widely used as a selective radiotracer in animal and human positron emission tomography (PET) imaging studies of the μ-opioid system due to its high affinity for receptors.
According to an Associated Press article from 2016, “Chemical weapon for sale: China’s unregulated narcotic”, fentanyl, carfentanil and other highly potent derivatives of fentanyl were actively marketed by several Chinese chemical companies.
Carfentanil was not a controlled substance in China until 1 March 2017, and until then was manufactured legally and sold openly over the Internet.
Authorities in Latvia and Lithuania reported seizing carfentanil as an illicit drug in the early 2000s. Around 2016, the US and Canada started reporting a dramatic increase in shipment of carfentanil and other strong opioid drugs to customers in North America from Chinese chemical supply firms.
In June 2016 the Royal Canadian Mounted Police seized one kilogram of carfentanil shipped from China in a box labeled “printer accessories”. According to the Canada Border Services Agency, the shipment contained 50 million lethal doses of the drug, more than enough to wipe out the entire population of the country, in containers labeled as toner cartridges for Hewlett-Packard LaserJet printers.
Allan Lai, an officer-in-charge at the Royal Canadian Mounted Police in Calgary who helped oversee the criminal investigation said, “With respect to carfentanil, we don’t know why a substance of that potency is coming into our country.”
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